Vázquez-Tato M Pilar, Mena-Menéndez Alberto, Feás Xesús, Seijas Julio A
Department of Organic Chemistry, Faculty of Science, University of Santiago de Compostela, E-27002 Lugo, Spain.
Int J Mol Sci. 2014 Feb 21;15(2):3287-98. doi: 10.3390/ijms15023287.
Ammonium trichloro[1,2-ethanediolato-O,O']-tellurate (AS101) is the most important synthetic Te compound from the standpoint of its biological activity. It is a potent immunomodulator with a variety of potential therapeutic applications and antitumoral action in several preclinical and clinical studies. An experimental design has been used to develop and optimize a novel microwave-assisted synthesis (MAOS) of the AS101. In comparison to the results observed in the literature, refluxing Te(IV) chloride and ethylene glycol in acetonitrile (Method A), or by refluxing Te(IV) chloride and ammonium chloride in ethylene glycol (Method B), it was found that the developed methods in the present work are an effective alternative, because although performance slightly decreases compared to conventional procedures (75% vs. 79% by Method A, and 45% vs. 51% by Method B), reaction times decreased from 4 h to 30 min and from 4 h to 10 min, by Methods A and B respectively. MAOS is proving to be of value in the rapid synthesis of compounds with new and improved biological activities, specially based on the benefit of its shorter reaction times.
三氯[1,2 - 乙二醇根合 -O,O']碲酸铵（AS101）从其生物活性的角度来看是最重要的合成碲化合物。在多项临床前和临床研究中，它是一种具有多种潜在治疗应用和抗肿瘤作用的强效免疫调节剂。已采用一种实验设计来开发和优化AS101的新型微波辅助合成法（MAOS）。与文献中观察到的结果相比，即在乙腈中回流四氯化碲和乙二醇（方法A），或在乙二醇中回流四氯化碲和氯化铵（方法B），发现本工作中开发的方法是一种有效的替代方法，因为尽管与传统方法相比性能略有下降（方法A为75%对79%，方法B为45%对51%），但反应时间分别从4小时减少到30分钟（方法A）和从4小时减少到10分钟（方法B）。事实证明，微波辅助合成法在快速合成具有新的和改进的生物活性的化合物方面具有价值，特别是基于其反应时间较短的优势。
